Single- and Multiple-Dose Pharmacokinetics of a Novel Tetramethylpyrazine Reservoir-Type Transdermal Patch versus Tetramethylpyrazine Phosphate Oral Tablets in Healthy Normal Volunteers, and in Vitro/in Vivo Correlation
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- Shen Teng
- Key Laboratory of Smart Drug Delivery, Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University
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- Xu Huinan
- Key Laboratory of Smart Drug Delivery, Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University
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- Weng Weiyu
- School of Pharmacy, East China University of Science and Technology
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- Zhang Jianfang
- Key Laboratory of Smart Drug Delivery, Ministry of Education & PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University
書誌事項
- タイトル別名
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- Single- and Multiple-Dose Pharmacokinetics of a Novel Tetramethylpyrazine Reservoir-Type Transdermal Patch <i>versus</i> Tetramethylpyrazine Phosphate Oral Tablets in Healthy Normal Volunteers, and <i>in Vitro</i>/<i>in Vivo</i> Correlation
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抄録
A novel reservoir-type transdermal system of 2,3,5,6-tetramethylpyrazine (TMP) was developed containing eucalyptus oil as a penetration enhancer. The single and multiple-dose pharmacokinetic profiles of TMP administrated by TMP transdermal patch were characterized in healthy volunteers using an in vivo, randomized, open-label, two-way crossover design. 2,3,5,6-Tetramethylpyrazine phosphate (TMPP) oral tablets were chosen as reference. Following single/multiple oral administration of 200/100 mg TMPP tablets, a TMP Cmax of 1284/613.5 ng/mL was observed within 0.75 h. Single/multiple applications of the TMP patch yielded mean Cmax of 309/325 ng/mL at a median Tmax of 5/4 h, with steady state achieved at second application. The mean Cmin of the patch was 131±30.38 ng/mL, contrasting to nearly zero for the tablet. Multiple applications of patch produced an accumulative effect over single application. At steady state 250 mg/20 cm2 TMP patch given daily provided comparable exposure to 100 mg TMPP tablets three times daily (3753.91 versus 3563.67 ng·h/mL). TMP tablets and patch yielded similar steady-state plasma concentrations: Cav (148.48±51.27, 156.41±40.31 ng/mL). The results demonstrated that TMP patch can achieve a therapeutic effect that is comparable to oral administration, exhibited prolonged and sustained plasma levels, fewer drug fluctuations, lower adverse effects, more convenience, and improved patient compliance. In-vitro permeation through human skin demonstrated zero-order kinetics with the flux of 364 µg/cm2/h. The predicted Cav (163.9 ng/mL) was in agreement with the observed Cav (156.4 ng/mL).
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 36 (6), 931-937, 2013
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679610004480
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- NII論文ID
- 130003361456
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- NII書誌ID
- AA10885497
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- COI
- 1:STN:280:DC%2BC3svotFamtA%3D%3D
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- ISSN
- 13475215
- 09186158
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- NDL書誌ID
- 024524306
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- PubMed
- 23514701
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 使用不可